PMID: 

Nat Prod Res. 2018 Oct 22:1-4. Epub 2018 Oct 22. PMID: 30345819

Abstract Title: 

Licochalcone B, a chalcone derivative from Glycyrrhiza inflata, as a multifunctional agent for the treatment of Alzheimer's disease.

Abstract: 

Licochalcone B (LCB), an extract from the root of Glycyrrhiza inflate, has the same caffeic acid scaffold as curcumin (Cur), which is known as an anti-Alzheimer's disease (AD) agent. However, there is no relevant research about anti-AD activity of LCB. In this study, the anti-AD activity of LCB was investigated. LCB could inhibit amyloid beta (Aβ) self-aggregation (IC = 2.16 ± 0.24 μM) and disaggregate pre-formed Aβfibrils, reduce metal-induced Aβaggregation through chelating metal ions. Molecular docking further revealed that LCB inhibited Aβself-aggregation through forming two hydrogen bonds with Lys28 to block the salt bridge interaction at the C-terminus of Aβ. Anti-oxidant property of LCB was also observed by DCFH-DA assay. In addition, LCB did show neuroprotective activity against HO-induced cell death in SH-SY5Y cells. In general, our results demonstrate that LCB, as a multifunctional agent, is likely to be promising therapeutics for AD.

read more

PMID: 

Crit Rev Food Sci Nutr. 2018 Mar 4 ;58(4):568-574. Epub 2017 Oct 4. PMID: 27469428

Abstract Title: 

Ursolic acid, a potential anticancer compound for breast cancer therapy.

Abstract: 

There are growing interests in the health benefits associated with consumption of fruits and vegetables, especially for the prevention of cancer, cardiovascular, or other chronic diseases. Epidemiological studies and clinical trials suggest that these health benefits are strongly associated with phytochemicals found in fruits and vegetables. Ursolic acid is a naturally synthesized pentacyclic triterpenoid, widely distributed in different fruits and vegetables. Current research suggested that ursolic acid and its derivatives exhibited anticancer activity, anti-inflammatory effects, and induction of apoptosis in several human cancer cells. In particular, ursolic acid inhibited breast cancer proliferation by inducing cell G1/G2 arrest and regulating the expression of key proteins in signal transduction pathways. In addition, ursolic acid induced apoptosis in human breast cancer cells through intrinsic and extrinsic apoptotic pathways. Ursolic acid was also determined to scavenge free radicals and have potent anti-inflammation activity. The purpose of this paper is to review recent literature on anticancer activity of ursolic acid and focus on its mechanisms of action.

read more

PMID: 

J Antibiot (Tokyo). 2020 Feb 12. Epub 2020 Feb 12. PMID: 32051569

Abstract Title: 

Antimicrobial and antibiofilm activities of ursolic acid against carbapenem-resistant Klebsiella pneumoniae.

Abstract: 

Previous studies demonstrated that ursolic acid (UA) present in apple pomace displays antimicrobial activity against some microorganisms, but the underlying mechanisms associated with this activity remain unexplored. Furthermore, there are no reports on the effect of UA on carbapenem-resistant Klebsiella pneumoniae (CRKP). This study examined the antimicrobial activity and mode of action of UA against CRKP was examined. Minimum inhibitory concentration (MIC) of UA against CRKP was determined by the agar dilution method. Variations in the intracellular pH (pHin), ATP concentration, and cell membrane potential were measured to assess the influence of UA on the cell membrane. Our results show that UA was effective against CRKP at an MIC of 0.8 mg ml. UA disrupted the cell membrane integrity of CRKP, exhibited strong inhibitory effects against biofilm formation and biofilm-related gene expression, and inactivated CRKP cells encased in biofilms. Thus, UA shows promise for use in combination with other antibiotics to treat multidrug resistant K. pneumoniae infections.

read more

PMID: 

Biomaterials. 2020 Jan 31 ;238:119828. Epub 2020 Jan 31. PMID: 32045781

Abstract Title: 

Magnesium and vitamin C supplementation attenuates steroid-associated osteonecrosis in a rat model.

Abstract: 

Magnesium (Mg)-based biometal attracts clinical applications due to its biodegradability and beneficial biological effects on tissue regeneration, especially in orthopaedics, yet the underlying anabolic mechanisms in relevant clinical disorders are lacking. The present study investigated the effect of magnesium (Mg) and vitamin C (VC) supplementation for preventing steroid-associated osteonecrosis (SAON) in a rat experimental model. In SAON rats, 50 mg/kg Mg, or 100 mg/kg VC, or combination, or water control was orally supplemented daily for 2 or 6 weeks respectively. Osteonecrosis was evaluated by histology. Serum Mg, VC, and bone turnover markers were measured. Microfil-perfused samples prepared for angiography and trabecular architecturewere evaluated by micro-CT. Primary bone marrow cells were isolated from each group to evaluate their potentials in osteoblastogenesis and osteoclastogenesis. The mechanisms were tested in vitro. Histological evaluation showed SAON lesions in steroid treated groups. Mg and VC supplementation synergistically reduced the apoptosis of osteocytes and osteoclast number, and increased osteoblast surface. VC supplementation significantly increased the bone formation marker PINP, and the combination significantly decreased the bone resorption marker CTX. TNFα expression and oxidative injury were decreased in bone marrow in Mg/VC/combination group. Mg significantly increased the blood perfusion in proximal tibia and decreased the leakage particles in distal tibia 2 weeks after SAON induction. VC significantly elevated the osteoblast differentiation potential of marrow cells and improved the trabecular architecture. The combination supplementation significantly inhibited osteoclast differentiation potential of marrow cells. In vitro study showed promoting osteoblast differentiation effect of VC, and anti-inflammation and promoting angiogenesis effect of Mg with underlying mechanisms. Mg andVC supplementation could synergistically alleviate SAON in rats, indicating great translational potentials of metallic minerals for preventing SAON.

read more

PMID: 

Bioorg Med Chem Lett. 2011 Jan 1 ;21(1):294-8. Epub 2010 Nov 5. PMID: 21123068

Abstract Title: 

Chalcones as novel influenza A (H1N1) neuraminidase inhibitors from Glycyrrhiza inflata.

Abstract: 

The emergence of highly pathogenic influenza A virus strains, such as the new H1N1 swine influenza (novel influenza), represents a serious threat to global human health. During our course of an anti-influenza screening program on natural products, one new licochalcone G (1) and seven known (2-8) chalcones were isolated as active principles from the acetone extract of Glycyrrhiza inflata. Compounds 3 and 6 without prenyl group showed strong inhibitory effects on various neuraminidases from influenza viral strains, H1N1, H9N2, novel H1N1 (WT), and oseltamivir-resistant novel H1N1 (H274Y) expressed in 293T cells. In addition, the efficacy of oseltamivir with the presence of compound 3 (5μM) was increased against H274Y neuraminidase. This evidence of synergistic effect makes this inhibitor to have a potential possibility for control of pandemic infection by oseltamivir-resistant influenza virus.

read more

PMID: 

Nutrients. 2020 Feb 7 ;12(2). Epub 2020 Feb 7. PMID: 32046183

Abstract Title: 

Extract Enhances Energy Expenditure via Improving Mitochondrial Function in Adipose Tissue and Skeletal Muscle.

Abstract: 

Withania somnifera (WS), commonly known as ashwagandha, possesses diverse biological functions. WS root has mainly been used as an herbal medicine to treat anxiety and was recently reported to have an anti-obesity effect, however, the mechanisms underlying its action remain to be explored. We hypothesized that WS exerts its anti-obesity effect by enhancing energy expenditure through improving the mitochondrial function of brown/beige adipocytes and skeletal muscle. Male C57BL/6J mice were fed a high-fat diet (HFD) containing 0.25% or 0.5% WS 70% ethanol extract (WSE) for 10 weeks. WSE (0.5%) supplementation significantly suppressed the increases in body weight and serum lipids, and lipid accumulation in the liver and adipose tissue induced by HFD. WSE supplementation increased oxygen consumption and enhanced mitochondrial activity in brown fat and skeletal muscle in the HFD-fed mice. In addition, it promoted browning of subcutaneous fat by increasing mitochondrial uncoupling protein 1 (UCP1) expression. Withaferin A (WFA), a major compound of WS, enhanced the differentiation of pre-adipocytes into beige adipocytes and oxygen consumption in C2C12 murine myoblasts. These results suggest that WSE ameliorates diet-induced obesity by enhancing energy expenditure via promoting mitochondrial function in adipose tissue and skeletal muscle, and WFA is a key regulator in this function.

read more

PMID: 

Molecules. 2011 Jul 6 ;16(7):5720-34. Epub 2011 Jul 6. PMID: 21734629

Abstract Title: 

Licocalchone-C extracted from Glycyrrhiza glabra inhibits lipopolysaccharide-interferon-γ inflammation by improving antioxidant conditions and regulating inducible nitric oxide synthase expression.

Abstract: 

The genus Glycyrrhiza consists of about 30 species, amoung these, G. glabra is the source of several phenolic compounds, known as flavonoids, such as licoagrodin, licoagrochalcones, licoagroaurone and licochalcone C, kanzonol Y, glyinflanin B and glycyrdione A, which have shown various pharmacological activities, including antitumor, antiparasitic, antileishmanial, anti-ulcer and antioxidative effects. Among these compounds, licochalcone C was isolated but its biology has not been fully examined. In our study we reproduced an inflammatory state by treating THP-1 (human myelomonocytic leukaemia) cells with pro-inflammatory stimuli, such as LPS and IFN-γ and we investigated the possible antioxidant activity of licochalcone C at a concentration of 50 μM. Our results show that treatment with licochalcone C attenuates the LPS-IFN-γ-induced inflammatory response by significantly decreasing the expression and activity of iNOS via NFκB (nuclear factor kappa-B), by influencing extracellular O₂⁻ production, and by modulating the antioxidant network activity of SOD (superoxide dismutase), CAT (catalase) and GPx (glutathione peroxidase) activity. Based on these results we hypothesize that Licochalcone C has antioxidant properties since it reduces the production of superoxide radicals and consequently reduces the activity of iNOS.

read more

A simple natural food supplement has been shown to significantly enhance well-being and reduce the difficulty of bathroom urgency that often comes along with ulcerative colitis

PMID: 

J Microbiol Biotechnol. 2012 Jun ;22(6):800-5. PMID: 22573157

Abstract Title: 

Antimicrobial activity of licochalcone E against Staphylococcus aureus and its impact on the production of staphylococcal alpha-toxin.

Abstract: 

Licochalcone E was firstly isolated from licorice root in 2005, which belongs to the retrochalcone family. Studies on the biological activities of licochalcone E were in the initial stage. In the study, we demonstrated that licochalcone E has potent antimicrobial property against Staphylococcus aureus. Furthermore, via hemolysis, Western blot, and real-time RT-PCR assays, we have shown that subinhibitory concentrations of licochalcone E dosedependently reduces the production of alpha-toxin in both methicillin-sensitive S. aureus (MSSA) and methicillinresistant S. aureus (MRSA). The data suggest that licochalcone E may deserve further investigation as a potential therapeutic against S. aureus infections, or the structure of licochalcone E may be used as a basis for chemical synthesis of novel anti-S. aureus compounds.

read more

PMID: 

Cancer Prev Res (Phila). 2013 Jun ;6(6):603-13. Epub 2013 Apr 26. PMID: 23625311

Abstract Title: 

Licochalcone E present in licorice suppresses lung metastasis in the 4T1 mammary orthotopic cancer model.

Abstract: 

We investigated whether licochalcone E (LicE), a phenolic constituent of licorice, inhibits mammary tumor growth and metastasis using animal and cell culture models. 4T1 mammary carcinoma cells were injected into the mammary fat pads of syngeneic BALB/c mice. Starting 7 days after the injection, the mice received LicE (7 or 14 mg/kg body weight/day) via oral gavage for 25 days. LicE suppressed solid tumor growth and lung metastasis, but did not exhibit kidney or liver toxicity. In tumor tissues, LicE treatment induced a reduction in the expression of Ki67, cyclins, and cyclin-dependent kinases and stimulated apoptosis with increased expression of Bax and cleaved caspase-3 but decreased expression of Bcl-2. In addition, LicE decreased expression of CD31, vascular endothelial growth factor (VEGF)-A and C, VEGF-receptor 2, lymphatic vessel endothelial receptor-1, CD45, cyclooxygenase-2, inducible nitric oxide synthase, and hypoxia inducible factor-1α in tumor tissues. In lung tissues, LicE reduced the levels of proinflammatory cytokines and angiogenesis/metastasis-related proteins. In mammary cancer cell cultures, LicE (5-20 μmol/L) dose dependently inhibited cell migration and invasion. LicE inhibited secretion of matrix metalloproteinase-9, urokinase-type plasminogen activator and VEGF-A, and stimulated secretion of tissue inhibitor of metalloproteinase-2 in MDA-MB-231 cells. In addition, LicE inhibited tube formation of vascular endothelial cells. We show that LicE administration suppressed tumor growth and lung metastasis in the mouse model in conjunction with LicE inhibition of cell migration, invasion, and tube formation in vitro. Reduced tumor growth and metastasis in LicE-treated mice may be, at least in part, attributed to reduced inflammation and tumor angiogenesis.

read more